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WO/2003/047499A2 |
An amphiphilic compound is provided capable of forming vesicles or liposomes, said amphiphilic compound having at least one headgroup containing a selectively cleavable group or moiety such as a residue of a choline or phenylalanine deri...
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WO/2003/045967A1 |
This invention is directed to compounds of formula (1) and their pharmaceutically acceptable salts, wherein R?1¿, R?2¿, and R?3¿ are as defined herein; intermediates for the synthesis of such compounds; and methods of using such compo...
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WO/2003/035661A1 |
The invention relates to compounds having the following formula (I), in which: R¿a? represents a sugar moiety, an arylamino group, or an alkyl group comprising at least one amino group, R¿b? represents an halogen atom, an halogenoalkyl...
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WO2003000709A9 |
the invention relates to Siglec inhibitors that have an increased affinity for the receptor molecule. The Siglec inhibitors provided by the invention are preferably selective of a given Siglec molecule. The invention further relates to m...
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WO/2003/022860A1 |
Preparation of synthetic monosaccharides, disaccharides, trisaccharides, tetrasaccharides and pentasaccharides for use in the preparation of synthetic heparinoids.
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WO/2003/018598A2 |
Monosaccharide (pyranoside) conjugates of the formula have been found to be useful as enhancers and/or inhibitors of heparin binding to FGF. The compounds have the potential to be useful in regenerative medicine or for treatment of patho...
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WO/2003/011881A2 |
Glucoside and glucuronide derivatives ofhydromorphone, dihydromorphine, and dihydroisomorphine and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising a glucoside or glucuronide derivative ofhydromorphone, d...
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WO/2003/002127A1 |
The present invention relates to the use of a glycosidase inhibitor for the manufacture of a medicament for the treatment of a disease, wherein glycosidase enzymes hydrolyze glycoconjugates of a patient to reveal neutral glycan receptors...
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WO/2002/090359A1 |
The quaternary ammonium N-glucuronide adduct of 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethox
y)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine is cleavable by glucuronidase enzymes in the body and can thereby act as a...
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WO2001056563A9 |
The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advance...
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WO/2002/086116A1 |
An enzyme which decomposes a sulfated fucoglucuronomannan and is useful in the field of glycotechnology; a process for producing the enzyme; a fucoidan fraction reduced in the number of the kinds of molecules and useful as a reagent in g...
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WO/2002/083066A2 |
Crystalline complexes are obtained from a 1:1 or 2:1 mixtures of either the (D) or (L) enantiomer of natural amino acids and compounds of formula (I) wherein R¿1?, R¿2? and R¿2a? are independently hydrogen, OH, OR¿5?, alkyl, -OCHF?2Â...
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WO/2002/072593A2 |
The present invention relates to alkylated C-sugars which are now carbohydrate derivatives based on the 'C-Sugar' platform. These alkylated C-sugars are converted from hydrophilic, hydrogen-bonded saccharide derivatives and are very stab...
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WO/2002/072779A2 |
Nucleic acid labeling compounds are disclosed. The compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a ...
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WO/2002/064605A2 |
This invention provides $g(b)-D-Glucuronidase substrates of formula (I) wherein R¿1?, R¿2?, and R¿7? - R¿12? are independently selected from the group consisting of: hydrogen, fluorine, chlorine, bromine, iodine, alkyl, hydroxyl, alk...
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WO/2002/062810A2 |
Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLe?X¿) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in prep...
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WO/2002/053159A1 |
Tacrolimus derivatives having high levels of neurotrophic activity and low levels of immunosuppresive activity. These compounds are useful as neurotrophic agents, particularly, for preventing or treating neuronal injury/dysfunction.
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WO/2002/051828A2 |
The invention concerns novel C-glycoside derivatives, their synthesis methods and compositions containing them. The invention also concerns the use, in a physiologically acceptable medium, in a cosmetic composition or for preparing a pha...
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WO/2002/051803A2 |
The invention concerns novel C-glycoside derivatives, cosmetic, hygienic or pharmaceutical compositions containing them and their use as amphiphilic agents and in particular as emulsifiers and/or surfactants. The invention also concerns ...
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WO/2002/048197A1 |
Primary hydroxyl groups in a substrate having both primary and secondary hydroxyl groups can be selectively oxidised to carbaldehyde and/or carboxyl groups by contacting the substrate with a cyclic nitroxyl compound in the presence of a ...
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WO/2002/040060A2 |
The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermedi...
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WO/2002/036600A2 |
In a composition comprising a therapeutic agent and a compound which is a trisaccharide or higher polysaccharide, that compound has the formula X[-Y-Z]¿n? wherein X and Z are each saccharide molecules in which none, some or all OH group...
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WO/2002/032963A1 |
This invention relates to compounds of general formula I, in which S is a carbohydrate core matrix; a is a pharmaceutically active moiety; L is a linker a covalent bond; n is an integer of 2 to 19; and R' is hydrogen, thioalkyl or X-Z in...
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WO/2002/032913A1 |
A method for the oxidation of substrates comprising treating an aqueous, basic solution of a substrate having an oxidizable functionality using an elemental halogen as terminal oxidant in the presence of an oxoammonium catalyst/halide co...
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WO/2002/030940A2 |
The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases Cls and Clr. The invention ...
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WO/2002/024832A1 |
The invention aims at providing a method for protecting unsaturated compounds from chemical changes due to radical reactions by inhibiting the conversion of unsaturated compounds into radicals. This aim is attained by an aggregate-formin...
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WO/2002/018449A1 |
The present invention provides a new class of compounds presenting a high compatibility with tissues and organic fluids. Such new compounds are polysaccharides essentially formed of units of uronic acid and/or hexosamine, containing nitr...
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WO/2002/010130A1 |
Processes for the preparation of pyrrolidones (7 and 8) and pyrrolidines (9 and 10) from tri-O-acetyl-D-erythro-4-pentulosonic acid esters are described. The compounds are aza sugar analogs of D-ribofuranoside and are intermediates to dr...
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WO/2002/008240A1 |
Compounds represented by the general formula (1) wherein R?1¿ is a carboxyl-protecting group; and R?2¿, R?3¿ and R ?4¿ are each independently a hydroxyl-protecting group, or alternatively R?2¿ and R?3¿ or R?3¿ and R?4¿ together r...
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WO/2002/008239A1 |
The invention relates to novel disaccharides of formula (I), wherein R?1¿ is selected from the group consisting of hydrogen, linear or branched (C¿1?-C¿4?) alkyl, phenylalkyl with less than ten carbon atoms and -COCH¿3?; R?2¿ is sel...
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WO/2002/004471A1 |
Hyaluronic acid oligosaccharides consisting of 4 to 60 saccharides; fractions characterized by containing these hyaluronic acid oligosaccharides and having specific physicochemical properties; and drugs containing the same. These hyaluro...
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WO/2002/002583A1 |
An amine salt of a lignan compound, i.e., [1-O-[4-(3,4-dimethoxyphenyl)-2-(3-ethylpentanoyl)-5,6,7-tri
methoxy-3-(methoxycarbonyl)naphthalen-1-yl]-$g(b)-D-glucopyr
anoside]uronic acid. The salt is useful as a medicine. Also provided is a...
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WO/2001/079244A1 |
Hydrophilic transportable N-linked glycosyl dopaminergic prodrug compounds according to FORMULA (V), wherein, Ring 1 comprises a cyclic or heterocyclic ring, or aryl or heteroaryl ring, all of said rings comprising 4 to 8 carbon atoms, a...
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WO/2001/074776A1 |
A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as ...
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WO/2001/044220A2 |
The present invention provides fluorescent nucleoside analogs which comprise a fluorescent cyclic compound joined to a carbon of a sugar molecule such as pentose, hexose, ribose or deoxyribose or analogs thereof in either an $g(a) or $g(...
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WO/2001/044264A2 |
The invention relates to compounds of formula (I), which are suitable for the production of medicaments for the treatment and prophylaxis of diseases, in which an increased activity of matrix-degrading enzymes, in particular, stromelysin...
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WO/2001/034657A1 |
In a new process for oxidising a primary and/or secondary alcohol, an oxidising agent is used in the presence of a di-tertiary-alkyl nitroxyl, in an aqueous reaction medium at a pH of below 7. The di-tertiary-alkyl nitroxyl is especially...
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WO/2001/027128A1 |
SGLT2 inhibiting compounds are provided having formula (I) where R?1¿, R?2¿, and R?2a¿ are independently hydrogen, OH, OR?5¿, lower alkyl, CF¿3?, OCHF¿2?, OCF¿3?, SR?5i¿ or halogen, or two of R?1¿, R?2¿ and R?2a¿ together with...
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WO/2001/025246A2 |
The current invention relates to the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including human) origin. In particular, this invention pr...
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WO/2001/022971A1 |
Sebum production inhibitors which contain as the active ingredient compounds having glucuronic acid derivatives and glucosamine derivatives in the structure as represented by general formula (1) or pharmacologically acceptable salts ther...
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WO/2001/019960A1 |
Chimeric carbohydrates produced by recombinant microorganism carrying exogenous glycosyl transferases act with or without exogenous enzymes required for synthesis or nucleotide synthesis precursors. These recombinant microorganism can be...
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WO1999061647A9 |
A process for purifying and concentrating a gluconic acid derivative, such as 2-keto-L-gulonic acid, comprising introducing a non-viable and/or acidified fermentation medium or an in-vitro reactor medium comprising at least the gluconic ...
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WO/2001/009152A1 |
The present invention relates to a process for the purification of 2-keto-L-gulonic acid by continuous liquid chromatography using a weakly basic ion exchange resin.
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WO/2001/000217A1 |
Medicinal compositions for preventing or treating diarrhea which contain, as the active ingredient, siastain B or its derivatives having a $g(b)-glucuronidase inhibitory activity and are useful as preventives or remedies for diarrhea whe...
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WO/2000/074674A1 |
What is disclosed is a meso-tetraarylporphyrin compound suitable for photodynamic therapy Forumula 1 or derivatives thereof, wherein two or three of R, R', R'', R''' represent cationic groups and the remaining R, R', R'', or R''' groups ...
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WO/2000/066601A1 |
The invention concerns a method for preparing aloin which consists in extracting from a substance containing aloe, in particular the yellow sap of aloe or a derived product, in the presence of an aliphatic diol or triol with low molecula...
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WO/2000/061568A2 |
The invention relates to substituted 1,4-benzothiazepine-1,1-dioxide derivatives and to the acid addition salts thereof. The invention discloses 1,4-benzothiazepine-1,1-dioxide derivatives of formula (I), wherein R?1¿, R?2¿, R?3¿ and ...
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WO/2000/061640A1 |
Crosslinked compounds of hyaluronic acid and the derivatives thereof, prepared by the technique of precipitation induced by supercritical antisolvent (SAS), can be used to advantage for the preparation of biomaterials for use in the fiel...
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WO/2000/060719A1 |
The invention concerns a generator for a windmill. The generator is of the kind being directly coupled to the main shaft of the wind rotor of the windmill. The generator is a stator consisting of a number of stator modules that are indiv...
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WO/2000/056734A1 |
The invention relates to compounds of formula (I), their tautomers, their salts and their water addition products, the radicals and symbols A, D, E, G and L having the meanings given in claim no. 1 and for example A = N, CR; D = C or N, ...
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